Pharmacology is the study of drugs and their effects. Anabolic pharmacology is the study of drugs that have a growth-promoting effect in muscle. This column will explore anabolic pharmacology by profiling a different anabolic drug and its effects each month. The focus of discussion this month will be the anabolic-androgenic steroid, Primobolan.
Methenolone is a synthetic derivative of dihydrotestosterone that is more commonly known by the trade name, Primobolan. The acetate ester version is taken orally, although there was once an injectable version of this ester. A highly-overlooked steroid, many people do not consider Primobolan to be very effective and coupled with its high price, do not consider it to be worthwhile. The oral form of methenolone is relatively weak due to the fact that methenolone is not 17-alpha alkylated. Instead, the 1-methyl group seems to offer some protection from metabolism to 1- and 2-hydroxy metabolites. Even so, the acetate does not have great oral bioavailability and a pretty high dose is needed to see significant effects.
Since it is a DHT derivative, methenolone does not aromatize nor does it have much progestational activity. In fact, being a DHT derivative, Primobolan likely acts as an aromatase inhibitor to some degree, which probably contributes to its reputation as a 'dry gainer' with less suppressive effects. Since it is already 5-alpha reduced, it does not get metabolized by 5-alpha reductase. Methenolone still undergoes metabolism by 3-alpha hydroxysteroid dehydrogenase in skeletal muscle, but less so than DHT.1 This results in a molecule that is somewhat less potent but still has a decent anabolic-to-androgenic ratio. Furthermore, it binds only moderately to sex hormone-binding globulin (SHBG), and there is no evidence that methenolone interacts to any degree with the glucocorticoid or progesterone receptors.2
Primobolan does not bring on massive weight gain, but this is due to the fact that there is very little water and fat accumulated. Primobolan is used for adding quality mass with little to no side effects, but the injectable version is much preferred over the oral version. Low doses of Primobolan have been used by women, with minimal side effects. Some have argued that Primobolan can be used without shutting down natural testosterone production. While suppression will be reduced with this steroid because it does not convert to estrogen, there will still be some reduction in testosterone production that will become worse as higher doses are used. A little-known fact about methenolone is that it has been shown to have similar levels of efficacy as oxymetholone for elevating red blood cell count.3 Methenolone the tablets or the injectable has never been as available as most of the other 'standbys,' and is often expensive when it is found. There are only a few pharmaceutical preparations available, and these items are often scarce— even from black-market sources.
Methenolone enanthate is the injectable form of this steroid, referred to as Primobolan Depot, its original trade name. The enanthate ester provides for a relatively slow release from the injection site and could be injected as infrequently as every 10 to 14 days, though most users will inject it weekly or even twice weekly. The injectable version of methenolone is much more effective than the oral version, since you do not have the effect of first-pass metabolism to contend with. Once the ester is stripped off, you have just the parent methenolone molecule.
The injectable version of methenolone with the enanthate ester is a potent steroid. It is usually injected on a weekly or sometimes shorter basis in doses of 400 to 600 milligrams for men and 50 to 100 milligrams for women. Women actually do better with a longer injection period of 10 to 12 days, to avoid a buildup in androgen levels. Methenolone is considered to be one of the safest steroids. Although methenolone is not C-17 alpha-alkylated, the 1-methyl group can cause some elevations in liver enzymes (even with the injectable)— but less so than the C-17 alkyl derivatives such as methandrostenolone. This is definitely not an 'instant gratification' drug, because it does not cause large amounts of water retention, and is less potent than other commonly-used injectables like nandrolone or even testosterone. Some people still prefer methenolone because even though it does not result in immediate gains, it generally doesn't produce as many side effects as other drugs.
References:
1. Schanzer W: Metabolism of anabolic androgenic steroids. Clin Chem, Jul;42(7):1001-20, 1996.
2. Saartok T, Dahlberg E, Gustafsson JA: Relative binding affinity of anabolic-androgenic steroids: comparison of the binding to the androgen receptors in skeletal muscle and in prostate, as well as to sex hormone-binding globulin. Endocrinology, Jun;114(6):2100-6, 1984.
3. Gorshein D, Murphy S, Gardner FH. Comparative study on the erythropoietic effects of androgens and their mode of action. J Appl Physiol, 35(3):276-8, 1973.
Methenolone is a synthetic derivative of dihydrotestosterone that is more commonly known by the trade name, Primobolan. The acetate ester version is taken orally, although there was once an injectable version of this ester. A highly-overlooked steroid, many people do not consider Primobolan to be very effective and coupled with its high price, do not consider it to be worthwhile. The oral form of methenolone is relatively weak due to the fact that methenolone is not 17-alpha alkylated. Instead, the 1-methyl group seems to offer some protection from metabolism to 1- and 2-hydroxy metabolites. Even so, the acetate does not have great oral bioavailability and a pretty high dose is needed to see significant effects.
Since it is a DHT derivative, methenolone does not aromatize nor does it have much progestational activity. In fact, being a DHT derivative, Primobolan likely acts as an aromatase inhibitor to some degree, which probably contributes to its reputation as a 'dry gainer' with less suppressive effects. Since it is already 5-alpha reduced, it does not get metabolized by 5-alpha reductase. Methenolone still undergoes metabolism by 3-alpha hydroxysteroid dehydrogenase in skeletal muscle, but less so than DHT.1 This results in a molecule that is somewhat less potent but still has a decent anabolic-to-androgenic ratio. Furthermore, it binds only moderately to sex hormone-binding globulin (SHBG), and there is no evidence that methenolone interacts to any degree with the glucocorticoid or progesterone receptors.2
Primobolan does not bring on massive weight gain, but this is due to the fact that there is very little water and fat accumulated. Primobolan is used for adding quality mass with little to no side effects, but the injectable version is much preferred over the oral version. Low doses of Primobolan have been used by women, with minimal side effects. Some have argued that Primobolan can be used without shutting down natural testosterone production. While suppression will be reduced with this steroid because it does not convert to estrogen, there will still be some reduction in testosterone production that will become worse as higher doses are used. A little-known fact about methenolone is that it has been shown to have similar levels of efficacy as oxymetholone for elevating red blood cell count.3 Methenolone the tablets or the injectable has never been as available as most of the other 'standbys,' and is often expensive when it is found. There are only a few pharmaceutical preparations available, and these items are often scarce— even from black-market sources.
Methenolone enanthate is the injectable form of this steroid, referred to as Primobolan Depot, its original trade name. The enanthate ester provides for a relatively slow release from the injection site and could be injected as infrequently as every 10 to 14 days, though most users will inject it weekly or even twice weekly. The injectable version of methenolone is much more effective than the oral version, since you do not have the effect of first-pass metabolism to contend with. Once the ester is stripped off, you have just the parent methenolone molecule.
The injectable version of methenolone with the enanthate ester is a potent steroid. It is usually injected on a weekly or sometimes shorter basis in doses of 400 to 600 milligrams for men and 50 to 100 milligrams for women. Women actually do better with a longer injection period of 10 to 12 days, to avoid a buildup in androgen levels. Methenolone is considered to be one of the safest steroids. Although methenolone is not C-17 alpha-alkylated, the 1-methyl group can cause some elevations in liver enzymes (even with the injectable)— but less so than the C-17 alkyl derivatives such as methandrostenolone. This is definitely not an 'instant gratification' drug, because it does not cause large amounts of water retention, and is less potent than other commonly-used injectables like nandrolone or even testosterone. Some people still prefer methenolone because even though it does not result in immediate gains, it generally doesn't produce as many side effects as other drugs.
References:
1. Schanzer W: Metabolism of anabolic androgenic steroids. Clin Chem, Jul;42(7):1001-20, 1996.
2. Saartok T, Dahlberg E, Gustafsson JA: Relative binding affinity of anabolic-androgenic steroids: comparison of the binding to the androgen receptors in skeletal muscle and in prostate, as well as to sex hormone-binding globulin. Endocrinology, Jun;114(6):2100-6, 1984.
3. Gorshein D, Murphy S, Gardner FH. Comparative study on the erythropoietic effects of androgens and their mode of action. J Appl Physiol, 35(3):276-8, 1973.
